| Identification | Back Directory | [Name]
GS-9256 | [CAS]
1001094-46-7 | [Synonyms]
GS-9256
RFGUWOCFYCYEDM-ZOMNBDOOSA-N
Carbamic acid, N-[(2R,6S,13aR,14aS,16aS)-2-[[8-chloro-7-methoxy-2-[2-[(1-methylethyl)amino]-4-thiazolyl]-4-quinolinyl]oxy]-14a-[[(2,6-difluorophenyl)methyl]hydroxyphosphinyl]octadecahydro-5,16-dioxocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-6-yl]-, cyclopentyl ester | [Molecular Formula]
C46H56ClF2N6O8PS | [MOL File]
1001094-46-7.mol | [Molecular Weight]
957.461 |
| Hazard Information | Back Directory | [Uses]
GS-9256 is a selective HCV NS3 protease inhibitor. GS-9256 has good pharmacokinetic properties and antiviral activity[1]. | [in vivo]
GS-9256 (1 mg/kg, i.v., 30 min) is highly bioavailable in mice (near 100%) and moderately bioavailable in rats (14%), dogs (21%) and monkeys (14%). The elimination half-life is approximately 2 hours in mice, 0.6 hours in rats, 5 hours in dogs, and 4 hours in monkeys[1].
The pharmacokinetic parameters of GS-9256(IV, 2 mg/kg mouse and 1 mg/kg rat, dog, monkey; Oral, 50 mg/kg mouse, 5 mg/kg rat and monkey, 4 mg/kg dog)
| - | Parameters | CD-1 mouse | Sprague Dawley rat | Beagle dog | Cynomolgus monkey | | Intravenous | CL(L/h/kg) | 2.0 | 1.26 | 0.04 | 0.33 | | Vss (L/kg) | 2.3 | 0.16 | 0.09 | 0.27 | | t1/2(h) | 2.35 | 0.61 | 4.88 | 3.95 | | MRT(h) | 1.15 | 0.13 | 2.11 | 0.82 | Oral | Tmax(h) | 3.00 | 0.67 | 2.00 | 2.67 | | Cmax(nM) | 11116 | 265 | 4369 | 604 | | t1/2(h) | 1.31 | 0.53 | 4.22 | 4.42 | | AUC0-∞(nM*h) | 58959 | 445 | 21043 | 2304 | | F(%) | Complete | 13.9 | 21 | 14 |
| [References]
[1] Huiling Yang, et al. Preclinical characterization of the novel HCV NS3 protease inhibitor GS-9256. Antivir Ther. 2017;22(5):413-420. DOI:10.3851/IMP3132 |
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